Antifungal compound

Abstract

There is provided compound for use in therapy, the compound comprising repeating units of hydrophilic heterocyclic amine monomers that are coupled by hydrophobic linkers selected to confer a therapeutic effect. There is also provided the use of the above compound in the manufacture of a medicament for the treatment of a fungal infection and a method of treating a fungal infection using the above compound.

The invention claimed is: 
     
       1. A method of treating or preventing a fungal infection caused by  Aspergillus niger , comprising the step of administering an antifungal amount of a compound to a patient in need thereof, said compound having the general formula (I): 
       
         
           
           
               
               
           
         
         wherein: 
         R 1  and R 2  are each independently selected from aryl, arylalkyl, alkylarylalkyl, alkylaryl, alkyl, cycloalkyl, alkenyl or alkynyl, 
         said aryl, arylalkyl, alkylarylalkyl or alkylaryl being optionally substituted by alkyl, alkenyl or alkynyl; 
         each R 3  is independently selected from hydrogen, alkyl, alkenyl, alkynyl, aryl, cycloalkyl, heteroaryl, or heterocyclyl; 
         R 4  is selected from hydrogen or aryl, said aryl being optionally substituted by alkyl, alkenyl or alkynyl; 
            is either a single bond or a double bond; 
         q is an integer selected from 0 to 3; 
         m is an integer selected from 0 to 3; 
         p is an integer selected from 2 to 50; and 
         X −  is a counterion. 
       
     
     
       2. The method according to  claim 1 , wherein R 1  or R 2  are independently selected from aryl, arylalkyl or alkylarylalkyl. 
     
     
       3. The method according to  claim 1 , wherein R 1  or R 2  are independently selected from phenyl, phenylmethyl or methylphenylmethyl. 
     
     
       4. The method according to  claim 3 , wherein said phenyl, phenylmethyl or methylphenylmethyl is substituted at the ortho position or at the meta position. 
     
     
       5. The method according to  claim 1 , wherein R 2  is selected from C 1-6 -alkyl or C 2-6 -alkenyl. 
     
     
       6. The method according to  claim 5 , wherein R 2  is selected from the group consisting of methyl, ethyl, propyl, butyl, pentyl, hexyl, ethylene, propylene, butylene, pentylene or hexylene. 
     
     
       7. The method according to  claim 6 , wherein said hexylene is 3-hexenyl. 
     
     
       8. The method according to  claim 1 , wherein R 3  is selected from hydrogen. 
     
     
       9. The method according to  claim 1 , wherein R 4  is hydrogen or phenyl. 
     
     
       10. The method according to  claim 1 , wherein X is a halide selected from the group consisting of fluoride, iodide, bromide and chloride. 
     
     
       11. The method according to  claim 1 , wherein said compound of formula (I) has a molecular weight in the range of 1000 to 3000. 
     
     
       12. The method according to  claim 1 , wherein a compound of formula (I) is selected from formula (II) or formula (III): 
       
         
           
           
               
               
           
         
         wherein p is 6 to 20. 
       
     
     
       13. The method according to  claim 1  wherein said fungal infection is selected from keratitis or aspergillosis. 
     
     
       14. A method of reducing the fungal cell count on a fungal biofilm, comprising the step of administering an effective fungicidal amount of a compound selected to confer the fungicidal effect, said compound having the general formula (I): 
       
         
           
           
               
               
           
         
         wherein: 
         R 1  and R 2  are each independently selected from aryl, arylalkyl, alkylarylalkyl, alkylaryl, alkyl, cycloalkyl, alkenyl or alkynyl, 
         said aryl, arylalkyl, alkylarylalkyl or alkylaryl being optionally substituted by alkyl, alkenyl or alkynyl; 
         each R 3  is independently selected from hydrogen, alkyl, alkenyl, alkynyl, aryl, cycloalkyl, heteroaryl, or heterocyclyl; 
         R 4  is selected from hydrogen or aryl, said aryl being optionally substituted by alkyl, alkenyl or alkynyl; 
            is either a single bond or a double bond; 
         q is an integer selected from 0 to 3; 
         m is an integer selected from 0 to 3; 
         p is an integer selected from 2 to 50; and 
         X −  is a counterion.